64037-15-6Relevant academic research and scientific papers
Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB
Li, Dongsheng,Liu, Chao,Jiang, Xinhai,Lin, Yuan,Zhang, Jing,Li, Yan,You, Xuefu,Jiang, Wei,Chen, Minghua,Xu, Yanni,Si, Shuyi
, (2020/10/21)
N-(5-Chlorobenzo[d]oxazol-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamideox-amide has been identified as a potent inhibitor of Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.42 μM. In this study, a series of substituted 2-acylamide-1,3-zole analogues were designed and synthesized, and their anti-Mtb activities were analyzed. In total, 17 compounds were found to be potent anti-Mtb agents, especially against the MDR- and XDR-MTB strains, with MIC values 10 μM. These analogues can inhibit both drug-sensitive and drug-resistant Mtb. Four representative compounds were selected for further profiling, and the results indicate that compound 18 is acceptably safe and has favorable pharmacokinetic (PK) properties. In addition, this compound displays potent activity against Gram-positive bacteria, with MIC values in the range of 1.48–11.86 μM. The data obtained herein suggest that promising anti-Mtb candidates may be developed via structural modification, and that further research is needed to explore other compounds.
Substituted benzo - 1, 3 - [...] compound, its preparation and use
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Paragraph 0112; 0113, (2017/04/21)
The invention relates to a substituted benzo-1, 3-miscellaneous azole compound shown in the general formula I, and further relates to a preparation method of the compound and application to the preparation of antituberculosis drugs. The compound provided by the invention has effect not only on mycobacterium tuberculosis sensitive strains, but also on resistant strains which have drug resistance to isoniazid, rifampicin, and other traditional frontline antituberculosis drugs, and is a novel antimycobacterium tuberculosis compound.
A metal-free oxidative amination of benzoxazoles with primary amines and ammonia
Kloeckner, Ulrich,Weckenmann, Nicole M.,Nachtsheim, Boris J.
supporting information; experimental part, p. 97 - 100 (2012/02/03)
An efficient synthesis of 2-aminobenzoxazoles is described by a direct oxidative amination of unfunctionalized benzoxazoles with primary amines. The reaction could be performed in the absence of transition metals by using catalytic amounts of a quaternary ammonium iodide and tert-butylhydroperoxide as a cheap and easy-to-handle co-oxidant. In addition to primary amines, aqueous solutions of NH3 were used to introduce a primary amine group into the heterocyclic core. Georg Thieme Verlag Stuttgart. New York.
Cobalt- and manganese-catalyzed direct amination of azoles under mild reaction conditions and the mechanistic details
Kim, Ji Young,Cho, Seung Hwan,Joseph, Jomy,Chang, Sukbok
supporting information; experimental part, p. 9899 - 9903 (2011/02/25)
A bonding moment: A new cobalt- or manganese-catalyzed amination of azoles has been developed using peroxide and an acid additive to couple various types of azoles with ammonia, and primary or secondary amines (see scheme). The catalyst loadings are low, the optimal reaction conditions are mild, and the substrate scope is broad. The product azoles are an important pharmacophore of high biological activity. Copyright
Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182
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Page/Page column 16; 20, (2008/06/13)
The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-amin
6-11 Bridged oxime erythromycin derivatives
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Page/Page column 18, (2010/11/24)
The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes processes by which to make the compounds of the present invention.
6-11 Bridged oxime erythromycin derivatives
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Page/Page column 18-19, (2010/11/24)
The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes processes by which to make the compounds of the present invention.
